RIP1/RIP3/MLKL activator 1

Name: RIP1/RIP3/MLKL activator 1
Brand: MedChemExpress
SKU: HY-144828
Rating: 5.0 (6 reviews)

Cat. No.: HY-144828 Pureza: 97.0%: Ficha de datos
COA

SDS
Instrucciones de manejo
FAQs
Technical Support

RIP1/RIP3/MLKL activator 1 (Compound 6i) is a potent anti-glioma agent. RIP1/RIP3/MLKL activator 1 induces necroptosis through RIP1/RIP3/MLKL pathway. RIP1/RIP3/MLKL activator 1 exerts acceptable BBB permeability.

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RIP1/RIP3/MLKL activator 1 Estructura química

No. CAS : 2682850-41-3

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtener un presupuesto
500 mg	Obtener un presupuesto

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Revisión del cliente

Based on 6 publication(s) in Google Scholar

6 Publications Citing Use of MCE RIP1/RIP3/MLKL activator 1

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Ver todas las isoformas

RIPK1 RIPK2 RIPK3

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

IC₅₀ & Target

RIP1, RIP3, MLKL^[1]

In Vitro

RIP1/RIP3/MLKL activator 1 (Compound 6i) (96 h) shows antiproliferative activities in human glioma cell lines^[1].
RIP1/RIP3/MLKL activator 1 (0-4 μM, 0-72 h) exhibits remarkable antiproliferative activity for U251 cells in a time- and concentration-dependent manner^[1].
RIP1/RIP3/MLKL activator 1 (10 μM, 0-72 h) shows acceptable stability^[1].
RIP1/RIP3/MLKL activator 1 (0-2 μM, 24 h) effectively inhibits the migration of U251 cells^[1].
RIP1/RIP3/MLKL activator 1 induces necroptosis through RIP1/RIP3/MLKL pathway, and induces mitochondrial depolarization in U251 cells^[1].
RIP1/RIP3/MLKL activator 1 could not induce apoptosis in U251 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:	A172, LN229, U87, U251 and L02 cell lines
Concentration:	0-4 µM for U251 cells
Incubation Time:	96 h; 24, 48, and 72 h for U251 cells
Result:	Showed antiproliferative activity with IC₅₀ values of 3.03 ± 0.70, 1.78 ± 0.79, 1.22 ± 0.89, 0.94 ± 0.45, and 0.99 ± 0.46 µM against A172, LN229, U87, U251 and L02 cells, respectively. Time- and concentration-dependently inhibited the growth in U251 cells.

Western Blot Analysis^[1]

Cell Line:	U251
Concentration:	0, 0.5, 1, 2, and 4 µM
Incubation Time:	24 or 48 h
Result:	Concentration-dependently upregulated the expression of p-RIP1, RIP1, p-RIP3, RIP3, p-MLKL, and MLKL at 24 or 48 h.

In Vivo

RIP1/RIP3/MLKL activator 1 (Compound 6i) (2.50 ng/tail; i.v.; 48 h) inhibits U251 cell proliferation in vivo and exerts acceptable BBB permeability^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Zebrafish wide-type AB strain; 200 CM-DiI labeled U251 cells were transplanted into yolk sac of each wild-type zebrafish embryos at 2 dpf (2 days postfertilization)^[1]
Dosage:	2.50 ng/tail
Administration:	Microinjection; 48 h
Result:	Remarkably reduced the U251 xenografts fluorescence intensity.

Peso molecular

676.93

Fòrmula

C₄₃H₅₆N₄O₃

No. CAS

2682850-41-3

Appearance

Solid

Color

Orange to red

SMILES

CC1=C(C(C=C2C1=CC=C3[C@]4(CC[C@]5(CC[C@@](C(NCC6=CN(N=N6)CC7=CC=C(C=C7)C(C)(C)C)=O)(CC5[C@@]4(CC[C@@]23C)C)C)C)C)=O)O

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (147.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.4773 mL	7.3863 mL	14.7726 mL
5 mM	0.2955 mL	1.4773 mL	2.9545 mL
10 mM	0.1477 mL	0.7386 mL	1.4773 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad
Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.69 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.5 mg/mL (3.69 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureza y Documentación

Purity: 97.0%

Select Batch:

Ficha de datos (280 KB) SDS (393 KB)

COA (253 KB) HNMR (288 KB) MS (71 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Yao Feng, et al. Synthesis and biological evaluation of celastrol derivatives as potential anti-glioma agents by activating RIP1/RIP3/MLKL pathway to induce necroptosis. Eur J Med Chem. 2022 Feb 5;229:114070. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.4773 mL	7.3863 mL	14.7726 mL	36.9314 mL
	5 mM	0.2955 mL	1.4773 mL	2.9545 mL	7.3863 mL
	10 mM	0.1477 mL	0.7386 mL	1.4773 mL	3.6931 mL
	15 mM	0.0985 mL	0.4924 mL	0.9848 mL	2.4621 mL
	20 mM	0.0739 mL	0.3693 mL	0.7386 mL	1.8466 mL
	25 mM	0.0591 mL	0.2955 mL	0.5909 mL	1.4773 mL
	30 mM	0.0492 mL	0.2462 mL	0.4924 mL	1.2310 mL
	40 mM	0.0369 mL	0.1847 mL	0.3693 mL	0.9233 mL
	50 mM	0.0295 mL	0.1477 mL	0.2955 mL	0.7386 mL
	60 mM	0.0246 mL	0.1231 mL	0.2462 mL	0.6155 mL
	80 mM	0.0185 mL	0.0923 mL	0.1847 mL	0.4616 mL
	100 mM	0.0148 mL	0.0739 mL	0.1477 mL	0.3693 mL